Design, Synthesis and Characterization of Benzothiazole Analogues as Promising Pharmacological Agents

Abstract

Objective: Benzothiazole moiety containing various functional groups are found to have broad spectrum of biological activity and diverse chemical reactivity. The various pharmacological properties shown by the benzothiazole scaffolds were antitumor, anti-inflammatory, analgesic, antimicrobial, antileishmanial, anticonvulsant, and anti HIV properties. Keeping this in mind a series of (2-(benzo[ d ]thiazol-2-ylmethoxy)-5-substitutedphenyl) (substitutedphenyl) methanone scaffolds 4a–f has been designed, synthesized and characterized for suitable pharmacological properties. Methods: A series of (2-(benzo[ d ]thiazol-2-ylmethoxy)-5-substitutedphenyl) (substitutedphenyl) methanone scaffolds 4a–f has been synthesized by two steps chemical reactions by conventional stirring method at 40°C. Purification of the title compounds was achieved by silica gel flash column chromatography method. The characterization of the newly synthesized compounds was achieved by means of IR, NMR ( 1 H and 13 C) and HRMS methods. Results: The yield of the title compounds were found to be satisfactory in the range of 66–79%. Purity of the compounds were found up to 99.36% by HPLC method. Compounds 4a, 4b, 4c, 4d, and 4e were studied for single crystal X-ray studies and detailed interactions are reported. Conclusion: Reactions performed to achieve benzothiazole scaffolds 4a–f were environmentally friendly and yielded satisfactory purity and yield. The purified and characterized title compounds are proposed for suitable pharmacological activities in the following communication. Key words : Benzothiazole analogues, Synthesis, Pharmacological properties, Characterization, Antimosquito, Anti-HIV.